227275-02-7Relevant articles and documents
BENZAMIDE AND NICOTINAMIDE COMPOUNDS AND METHODS OF USING SAME
-
Paragraph 0167, (2015/07/15)
The present disclosure provides benzamide and nicotinamide compounds and pharmaceutical uses of the compounds. The compounds can be used to treat, for example, cancers such hematopoietic cancers (e.g., leukemia). The preferred compounds of the invention c
Studies on selectin blocker. 9. SARs of non-sugar selectin blocker against E-, P-, L-selectin bindings
Moriyama, Hideki,Hiramatsu, Yasuyuki,Kiyoi, Takao,Achiha, Toshio,Inoue, Yoshimasa,Kondo, Hirosato
, p. 1479 - 1491 (2007/10/03)
As a part of study of selectin blockers, we have already reported that a non-sugar selectin antagonist (3) was successfully discovered using a computational screening (Hiramatsu, Y.; Tsukida, T.; Nakai, Y.; Inou, Y.; Kondo, H.J. Med. Chem. 2000, 43, 1476). To investigate the SARs of compound 3 against E-, P-, and L-selectins, we synthesized the derivatives of compound 3 and evaluated their inhibitory activities toward selectin bindings. The structural diversity of compound 3 contained the following: (1) and modification of the spacer unit (4-7), (2) a modification of the tail (8-11), (3), a modification of the head unit (12-18). As a result, it was found that a non-sugar based selectin blocker (3) could be a potential lead compound for E-, P-, and L-selectin blockers and wome of the derivatives showed broad and/or selective inhibitory activities toward the E-, P-, and L-selectins. In addition, it was found that the experimental evidence well supported that the computational screening using 3D-pharmacophore model could be useful methodology to find out a new lead for the several type of selectin blockers, which included a broad and/or a selective inhibitor. Copyright